{"id":"gabexate","rwe":[{"pmid":"41847707","year":"2026","title":"The protease inhibitor gabexate mesylate targets Raf kinase inhibitor protein and reverses epithelial-mesenchymal transition in triple-negative breast cancer cells.","finding":"","journal":"Frontiers in oncology","studyType":"Clinical Study"},{"pmid":"41760056","year":"2026","title":"Aquaporin-4 (AQP4) antibody-positive neuromyelitis optica spectrum disorder (NMOSD) complicated with acute pancreatitis: A case report.","finding":"","journal":"Medicine","studyType":"Clinical Study"},{"pmid":"41391836","year":"2025","title":"Critical role of the mast cell/tryptase/PAR2 axis in anastrozole-induced pain.","finding":"","journal":"British journal of pharmacology","studyType":"Clinical Study"},{"pmid":"41240299","year":"2025","title":"Effects of Chromium-Niacin Supplementation on Production and Metabolic Performance in Transition Dairy Cows.","finding":"","journal":"Biological trace element research","studyType":"Clinical Study"},{"pmid":"40873760","year":"2025","title":"Arterial compliance is improved via enteral serine protease inhibition in experimental trauma/hemorrhagic shock.","finding":"","journal":"Frontiers in physiology","studyType":"Clinical Study"}],"tags":[{"label":"gabexate","category":"class"},{"label":"Small Molecule","category":"modality"},{"label":"Tryptase alpha/beta-1","category":"target"},{"label":"TPSAB1","category":"gene"},{"label":"HPN","category":"gene"},{"label":"PLAU","category":"gene"},{"label":"Active","category":"status"},{"label":"Anticoagulants","category":"pharmacology"},{"label":"Enzyme Inhibitors","category":"pharmacology"},{"label":"Hematologic Agents","category":"pharmacology"},{"label":"Protease Inhibitors","category":"pharmacology"},{"label":"Serine Proteinase Inhibitors","category":"pharmacology"}],"phase":"phase_3","safety":{},"trials":[],"aliases":[],"patents":[],"pricing":[],"allNames":["gabexate","gabexate mesilate","gabexate mesylate"],"offLabel":[],"synonyms":["gabexate","gabexate mesilate","gabexate mesylate"],"timeline":[],"approvals":[],"ecosystem":[],"mechanism":{"target":"Coagulation factor XII, Multidrug and toxin extrusion protein 1, Multidrug and toxin extrusion protein 2","targets":[{"gene":"TPSAB1","source":"DrugCentral","target":"Tryptase alpha/beta-1","protein":"Tryptase alpha/beta-1"},{"gene":"HPN","source":"DrugCentral","target":"Serine protease hepsin","protein":"Serine protease hepsin"},{"gene":"PLAU","source":"DrugCentral","target":"Urokinase-type plasminogen activator","protein":"Urokinase-type plasminogen activator"},{"gene":"SLC47A1","source":"DrugCentral","target":"Multidrug and toxin extrusion protein 1","protein":"Multidrug and toxin extrusion protein 1"},{"gene":"F2","source":"DrugCentral","target":"Prothrombin","protein":"Prothrombin"},{"gene":"SLC22A2","source":"DrugCentral","target":"Solute carrier family 22 member 2","protein":"Solute carrier family 22 member 2"},{"gene":"KLKB1","source":"DrugCentral","target":"Plasma kallikrein","protein":"Plasma kallikrein"},{"gene":"PLG","source":"DrugCentral","target":"Plasminogen","protein":"Plasminogen"},{"gene":"F12","source":"DrugCentral","target":"Coagulation factor XII","protein":"Coagulation factor XII"},{"gene":"F10","source":"DrugCentral","target":"Coagulation factor X","protein":"Coagulation factor X"}],"modality":"Small Molecule","drugClass":"gabexate","explanation":"Think of tryptase enzymes like scissors that cut through proteins. When these enzymes are overactive, they can cause problems in the body. GABEXATE acts like a brake, slowing down the scissors so they don't cut too much.","oneSentence":"GABEXATE works by inhibiting the activity of tryptase enzymes.","technicalDetail":"GABEXATE is a competitive inhibitor of tryptase alpha/beta-1, binding to the active site of the enzyme and preventing it from cleaving its substrates."},"commercial":{},"references":[{"id":1,"url":"https://drugcentral.org/drugcard/3257","fields":["approvals","synonyms","ATC","PK","indications","contraindications","DDIs","targets","patents","FAERS"],"source":"DrugCentral"},{"id":2,"url":"https://clinicaltrials.gov/search?intr=GABEXATE","fields":["trials"],"source":"ClinicalTrials.gov"},{"id":3,"url":"https://pubmed.ncbi.nlm.nih.gov/?term=GABEXATE","fields":["publications"],"source":"PubMed/NCBI"}],"_enrichedAt":"2026-03-30T13:45:34.122205","biosimilars":[],"competitors":[{"drugName":"amiloride","drugSlug":"amiloride","fdaApproval":"1981-10-05","genericCount":3,"patentStatus":"Off-patent — generic available","relationship":"same-target"}],"dataSources":[{"url":"https://drugcentral.org","name":"DrugCentral","fields":["indications","contraindications","safety","target","drugInteractions"],"retrievedDate":"2026-04-07"}],"genericName":"gabexate","indications":{"approved":[],"offLabel":[],"pipeline":[]},"drugCategory":"active","labelChanges":[],"relatedDrugs":[{"drugId":"amiloride","brandName":"amiloride","genericName":"amiloride","approvalYear":"1981","relationship":"same-target"}],"trialDetails":[{"nctId":"NCT06105580","phase":"NA","title":"Conduction System Pacing vs Biventricular Pacing in Systolic Dysfunction and Wide QRS: Mortality, Heart Failure Hospitalization or Cardiac Transplant","status":"RECRUITING","sponsor":"Hospital Clinic of Barcelona","startDate":"2023-11-27","conditions":["Cardiac Resynchronization Therapy","Heart Failure"],"enrollment":320,"completionDate":"2027-11"},{"nctId":"NCT06617247","phase":"EARLY_PHASE1","title":"Effects of Cannabidiol on Burnout Syndrome and Empathy of Caregivers of Older Adults","status":"NOT_YET_RECRUITING","sponsor":"University of Sao Paulo","startDate":"2024-12-01","conditions":["Burnout Syndrome"],"enrollment":26,"completionDate":"2026-12-31"},{"nctId":"NCT05033821","phase":"NA","title":"A Library-based Prevention Intervention for Adolescents Affected by Parental Drug Use","status":"COMPLETED","sponsor":"Johns Hopkins Bloomberg School of Public Health","startDate":"2022-07-08","conditions":["Substance Use","Sexual Behavior","Adolescent Behavior"],"enrollment":61,"completionDate":"2023-08-11"},{"nctId":"NCT02904629","phase":"NA","title":"Evaluation of Respecting the Circle of Life on Pregnancy Prevention Outcomes Among American Indian Adolescents","status":"COMPLETED","sponsor":"Johns Hopkins Bloomberg School of Public Health","startDate":"2016-05","conditions":["Sex","Unprotected Sex","Contraception","Alcohol Use","Drug Use","Pregnancy"],"enrollment":1072,"completionDate":"2022-04"},{"nctId":"NCT04426552","phase":"PHASE2","title":"Dexmedetomidine Versus Sevoflurane in Children With Anticipated Difficult Intubation","status":"UNKNOWN","sponsor":"Alexandria University","startDate":"2020-06-01","conditions":["Craniofacial Abnormalities","Mandibular Hypoplasia"],"enrollment":40,"completionDate":"2020-10-20"},{"nctId":"NCT03247803","phase":"NA","title":"Air-Q® SP Versus Williams Intubating Airway for Single-Operator FOI","status":"COMPLETED","sponsor":"University of Wisconsin, Madison","startDate":"2018-06-11","conditions":["Intubation; Difficult or Failed","Laryngeal Masks"],"enrollment":60,"completionDate":"2019-03-08"},{"nctId":"NCT02710266","phase":"PHASE3","title":"Evaluation of the Effect of Gabexate Mesilate in the Hepatocyte Protection After Liver Resection","status":"TERMINATED","sponsor":"Yonsei University","startDate":"2012-02-24","conditions":["Liver Disease"],"enrollment":2,"completionDate":"2017-02-25"},{"nctId":"NCT02501577","phase":"NA","title":"Comparison of Various Supraglottic Airway Devices for Fiberoptical Guided Tracheal Intubation","status":"UNKNOWN","sponsor":"University of Regensburg","startDate":"2015-03","conditions":["Intubation; Difficult"],"enrollment":30,"completionDate":"2015-10"},{"nctId":"NCT01910714","phase":"NA","title":"Adapting and Evaluating an EBI to Prevent HIV/AIDS Risk Among Apache Youth","status":"COMPLETED","sponsor":"Johns Hopkins Bloomberg School of Public Health","startDate":"2010-09","conditions":["HIV/AIDS"],"enrollment":267,"completionDate":"2013-09"}],"genericFilers":[],"latestUpdates":[],"manufacturing":[],"administration":{},"crossReferences":{"UNII":"4V7M9137X9","CHEBI":"CHEBI:31641","INN_ID":"3988","UMLSCUI":"C0085231","ChEMBL_ID":"CHEMBL87563","KEGG_DRUG":"D01672","DRUGBANK_ID":"DB12831","PUBCHEM_CID":"3447","IUPHAR_LIGAND_ID":"7863","SECONDARY_CAS_RN":"56974-61-9","MESH_DESCRIPTOR_UI":"D016670"},"formularyStatus":[],"_enricherVersion":"v2","developmentCodes":[],"ownershipHistory":[],"publicationCount":522,"therapeuticAreas":["Hematology"],"biosimilarFilings":[],"recentPublications":[{"date":"2026","pmid":"41847707","title":"The protease inhibitor gabexate mesylate targets Raf kinase inhibitor protein and reverses epithelial-mesenchymal transition in triple-negative breast cancer cells.","journal":"Frontiers in oncology"},{"date":"2026 Feb 27","pmid":"41760056","title":"Aquaporin-4 (AQP4) antibody-positive neuromyelitis optica spectrum disorder (NMOSD) complicated with acute pancreatitis: A case report.","journal":"Medicine"},{"date":"2025 Dec 14","pmid":"41391836","title":"Critical role of the mast cell/tryptase/PAR2 axis in anastrozole-induced pain.","journal":"British journal of pharmacology"},{"date":"2025 Nov 15","pmid":"41240299","title":"Effects of Chromium-Niacin Supplementation on Production and Metabolic Performance in Transition Dairy Cows.","journal":"Biological trace element research"},{"date":"2025","pmid":"40873760","title":"Arterial compliance is improved via enteral serine protease inhibition in experimental trauma/hemorrhagic shock.","journal":"Frontiers in physiology"}],"companionDiagnostics":[],"genericManufacturerList":[],"status":"active","brandName":"GABEXATE","companyName":"","companyId":"","modality":"Small molecule","firstApprovalDate":"","aiSummary":"GABEXATE is a small molecule drug in the gabexate class, targeting tryptase alpha/beta-1. It is not FDA-approved, and its commercial status is unknown. GABEXATE is used to treat conditions associated with excessive tryptase activity, although specific indications are not well-documented. As a gabexate, it is believed to inhibit the activity of tryptase enzymes, which play a role in various physiological and pathological processes. Further research is needed to fully understand its clinical applications and safety profile.","enrichmentLevel":3,"visitCount":0,"trialStats":{"total":0,"withResults":0},"verificationStatus":"partial","dataCompleteness":{"mechanism":true,"indications":false,"safety":false,"trials":true,"score":2}}